To provide an industrially advantageous method for safely producing a high-quality optically active 1H-3-aminopyrrolidine compound at low cost by using an optically active aspartic acid as a raw material.
This method for producing the optically active 1H-3- aminopyrrolidine compound is characterized by reacting an optically active amino-protected aspartic anhydride with a primary amine, subjecting the reaction product to cyclodehydration to obtain an optically active 1-aralkyl-3-(protected amino)pyrrolidine-2,5-dione compound, deprotecting the 3-position amino group of the compound to obtain an optically active 1-aralkyl-3-aminopyrrolidine-2,5- dione compound, successively reducing the carbonyl groups of the compound to obtain either an optically active 1-aralkyl-3-aminopyrrolidine compound or a salt thereof with a protonic acid, further subjecting the compound or the salt thereof to hydrogenolysis to obtain the optically active 1H-3- aminopyrrolidine compound or a protonic acid salt thereof.
NAKATO TAKESHI
TAKEHARA JUN
SUGANO KAZUAKI
ICHIKAWA SHUJI
